Instant green synthesis of silver nanoparticles using Terminalia chebula fruit extract and evaluation of their catalytic activity on reduction of methylene blue

A novel green approach for the synthesis and stabilization of silver nanoparticles (AgNPs) using water extract of Terminalia chebula (T. chebula) fruit under ambient conditions is reported in this article. The instant formation of AgNPs was analyzed by visual observation and UV–visible spectrophotometer. Further the effect of pH on the formation of AgNPs was also studied. The synthesized AgNPs were characterized by FT-IR, XRD, HR-TEM with EDS and DLS with zeta potential. Appearance of brownish yellow color confirmed the formation of AgNPs. In the neutral pH, the stability of AgNPs was found to be high. The stability of AgNPs is due to the high negative values of zeta potential and capping of phytoconstituents present in the T. chebula fruit extract which is evident from zeta potential and FT-IR studies. The XRD and EDS pattern of synthesized AgNPs showed their crystalline structure, with face centered cubic geometry oriented in (1 1 1) plane. HR-TEM and DLS studies revealed that the diameter of stable AgNPs was approximately 25 nm. Moreover the catalytic activity of synthesized AgNPs in the reduction of methylene blue was studied by UV–visible spectrophotometer. The synthesized AgNPs are observed to have a good catalytic activity on the reduction of methylene blue by T. chebula which is confirmed by the decrease in absorbance maximum values of methylene blue with respect to time using UV–visible spectrophotometer and is attributed to the electron relay effect.     

Green synthesis of silver nanoparticles using Andean blackberry fruit extract

Green synthesis of nanoparticles using various plant materials opens a new scope for the phytochemist and discourages the use of toxic chemicals. In this article, we report an eco-friendly and low-cost method for the synthesis of silver nanoparticles (AgNPs) using Andean blackberry fruit extracts as both a reducing and capping agent. The green synthesized AgNPs were characterized by various analytical instruments like UV–visible, transmission electron microscopy (TEM), dynamic light scattering (DLS), X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy. The formation of AgNPs was analyzed by UV–vis spectroscopy at λ_max = 435 nm. TEM analysis of AgNPs showed the formation of a crystalline, spherical shape and 12–50 nm size, whereas XRD peaks at 38.04°, 44.06°, 64.34° and 77.17° confirmed the crystalline nature of AgNPs. FTIR analysis was done to identify the functional groups responsible for the synthesis of the AgNPs. Furthermore, it was found that the AgNPs showed good antioxidant efficacy (>78%, 0.1 mM) against 1,1-diphenyl-2-picrylhydrazyl. The process of synthesis is environmentally compatible and the synthesized AgNPs could be a promising candidate for many biomedical applications.     

Antifungal potentiality of mycogenic silver nanoparticles capped with chitosan produced by endophytic Amesia atrobrunnea

This research reports the fabrication of silver nanoparticles (AgNPs) from endophytic fungus, Amesia atrobrunnea isolated from Ziziphus spina-christi (L.). Influencing factors for instance, thermal degree of incubation, media, pH, and silver nitrate (AgNO₃) molarity were optimized. Then, the AgNPs were encapsulated with chitosan (Ch-AgNPs) under microwave heating at 650 W for 90 s. Characterization of nanoparticles was performed via UV–visible (UV–vis) spectrophotometer, Fourier-transform infrared spectrophotometer (FTIR), zeta potential using dynamic-light scattering (DLS), and field-emission-scanning electron microscope (FE-SEM). Anti-fungal activity of Ch-AgNPs at (50, 25, 12.5, 6.25 mg/L) was tested against Fusarium oxysporum, Curvularia lunata, and Aspergillus niger using the mycelial growth inhibition method (MGI). Results indicated that Czapek-dox broth (CDB) with 1 mM AgNO₃, an acidic pH, and a temperature of 25–30 °C were the optimum for AgNPs synthesis. (UV–vis) showed the highest peak at 435 nm, whereas Ch-AgNPs showed one peak for AgNPs at 405 nm and another peak for chitosan at 230 nm. FTIR analysis confirmed that the capping agent chitosan was successfully incorporated and interacted with the AgNPs through amide functionalities. Z-potential was −19.7 mV for AgNPs and 38.9 mV for Ch-AgNPs, which confirmed the significant stability enhancement after capping. FES-SEM showed spherical AgNPs and a reduction in the nanoparticle size to 44.65 nm after capping with chitosan. The highest mycelial growth reduction using fabricated Ch-AgNPs was 93% for C. lunata followed by 77% for A. niger and 66% F. oxysporum at (50 mg/L). Biosynthesis of AgNPs using A. atrobrunnea cell-free extract was successful. Capping with chitosan exhibited antifungal activity against fungal pathogens.     

Green biosynthesis of silver nanoparticles from Annona squamosa leaf extract and its in vitro cytotoxic effect on MCF-7 cells

The biological method for the synthesis of silver nanoparticles (AgNPs) using Annona squamosa leaf extract and its cytotoxicity against MCF-7 cells are reported. The synthesized AgNPs using A. squamosa leaf extract was determined by UV–visible spectroscopy and it was further characterized by FT-IR, X-ray diffraction (XRD), Transmission electron microscopy (TEM), Zeta potential and energy dispersive spectrometric (EDS) analysis. The UV–visible spectrum showed an absorption peak at 444 nm which reflects surface plasmon resonance (SPR) of AgNPs. TEM photography showed biosynthesized AgNPs were predominantly spherical in shape with an average size ranging from 20 to 100 nm. The Zeta potential value of ?37 mV revealed the stability of biosynthesized AgNPs. Furthermore, the green synthesized AgNPs exhibited a dose-dependent cytotoxicity against human breast cancer cell (MCF-7) and normal breast epithelial cells (HBL-100) and the inhibitory concentration (IC₅₀) were found to be 50 μg/mL, 30 μg/mL, and 80 μg/mL, 60 μg/ml for AgNPs against MCF-7 and normal HBL-100 cells at 24 h and 48 h incubation respectively. An induction of apoptosis was evidenced by (AO/EtBr) and DAPI staining. Application of such eco-friendly nanoparticles makes this method potentially exciting for the large scale synthesis of nanoparticles.     

Green synthesis of silver nanoparticles with Dalbergia spinosa leaves and their applications in biological and catalytic activities

The phytosynthesis of silver nanoparticles (AgNPs) by Dalbergia spinosa leaves (DSL) in aqueous extract was investigated. AgNPs were characterized by UV–visible absorption spectroscopy (UV–vis), transmission electron microscopy (TEM) and Fourier transform infra red spectrophotometry (FTIR). The results showed that the increase in the initial extract concentration at room temperature increased the mean size and widened the size distribution of the AgNPs, leading to a red shift and broadening the surface plasmon resonance absorption (439 nm). The results showed that the reducing sugars and flavonoids were primarily responsible for the bioreduction of silver ions and that their reductive capability was promoted at 36 °C. TEM analysis showed that the AgNPs were nearly spherical in shape with an average size of 18 ± 4 nm. When evaluated for in vitro antioxidant activity by DPPH, NO, hydrogen peroxide radicals, reducing power and CUPRAC assay methods in addition to anti-inflammatory activity by HBRC method, the silver nanoparticles exhibited considerably enhanced antioxidant and anti-inflammatory activity at the test doses when compared with that of the standards and the plant extract. Finally, the antibacterial activity of the AgNPs against two Gram-positive bacteria and two Gram-negative bacteria showed moderate antibacterial activity when compared with the standard and the plant extract. The synthesized silver nanoparticles were also effective in the catalytic reduction of 4-nitrophenol (4-NP) into 4-aminophenol (4-AP).     

Extracellular biosynthesis of silver nanoparticles using Rhizopus stolonifer

Synthesis of silver nanoparticles (AgNPs) has become a necessary field of applied science. Biological method for synthesis of AgNPs by Rhizopus stolonifer aqueous mycelial extract was used. The AgNPs were identified by UV–visible spectrometry, X-ray diffraction (XRD), transmission electron microscopy (TEM) and Fourier transform infrared spectrometry (FT-IR). The presence of surface plasmon band around 420 nm indicates AgNPs formation. The characteristic of the AgNPs within the face-centered cubic (fcc) structure are indicated by the peaks of the X-ray diffraction (XRD) pattern corresponding to (1 1 1), (2 0 0) and (2 2 0) planes. Spherical, mono-dispersed and stable AgNPs with diameter around 9.47 nm were prepared and affirmed by high-resolution transmission electron microscopy (HR-TEM). Fourier Transform Infrared (FTIR) shows peaks at 1426 and 1684 cm⁻¹ that affirm the presence of coat covering protein the AgNPs which is known as capping proteins. Parameter optimization showed the smallest size of AgNPs (2.86 ± 0.3 nm) was obtained with 10⁻² M AgNO₃ at 40 °C. The present study provides the proof that the molecules within aqueous mycelial extract of R. stolonifer facilitate synthesis of AgNPs and highlight on value-added from R. stolonifer for cost effectiveness. Also, eco-friendly medical and nanotechnology-based industries could also be provided. Size of prepared AgNPs could be controlled by temperature and AgNO₃ concentration. Further studies are required to study effect of more parameters on size and morphology of AgNPs as this will help in the control of large scale production of biogenic AgNPs.     

Study of the interaction of human serum albumin with Alstonia scholaris leaf extract-mediated silver nanoparticles having bactericidal property

This study investigates the green synthesis of AgNPs from 1 mM aqueous AgNO₃ using 10% leaf extract of Alstonia scholaris (Chhatim) for its wide antibacterial and medicinal properties. The synthesized AgNPs were duly characterized by UV–vis (UV–vis) spectrophotometry, dynamic light scattering, field emission scanning electron microscopy, transmission electron microscopy, energy-dispersive analysis of X-rays spectroscopy, and fourier transform infrared spectrophotometry. Their antibacterial property was tested against Escherichia coli (ATCC 25922), and minimum inhibitory concentrations of 0.08 nM of AgNPs were obtained, which suggests improved therapeutic efficacy. We report the interaction of human serum albumin (HSA) with this nanoparticle, and this interaction was studied by UV–vis, fluorescence, and circular dichroism spectroscopies and zeta potential measurement at room temperature. It was found that the AgNPs form a complex with HSA, which may cause the slightest change in the conformation of HSA. The calculated values of Stern-Volmer quenching constant, binding constant, and binding distance were 1.82 × 10⁷ M⁻¹, 1.58 × 10⁷ M⁻¹, and 3.68 nm, respectively. Therefore, in future, the present study may provide useful information to design a better antibacterial compound by using green synthesized nanoparticles with fewer side effects.     

Green synthesized doxorubicin loaded zinc oxide nanoparticles regulates the Bax and Bcl-2 expression in breast and colon carcinoma

The green synthesis of zinc oxide nanoparticles (ZnONPs) using Borassus flabellifer fruit extract was characterized by UV–visible spectroscopy, FT-IR, XRD, TEM, Zeta potential and EDS analysis. The UV–visible spectrum showed an absorption peak at 368 nm that reflects surface Plasmon resonance (SPR) ZnONPs. TEM photograph showed that the green synthesized ZnONPs were porous in nature and rod like structure with an average size of 55 nm. The Zeta potential value of −21.5 mV revealed the surface charge of green synthesized ZnONPs. In this study, we examined the synthesized DOX-ZnONPs exhibited a dose-dependent cytotoxicity against MCF-7 and HT-29. The inhibitory concentration (IC₅₀) was found to be 0.125 μg mL⁻¹ for MCF-7 and HT-29 cells. An induction of apoptosis was evidenced by nuclear stain Hoechst 33258. In vivo toxicity assessment showed that DOX-ZnONPs have low systemic toxicity in murine model system. The results prove that the DOX-ZnONPs has low toxicity and high therapy efficacy, which provides convincing evidence for the green biosynthesized ZnO as a promising candidate for a drug delivery system.     

Facile synthesis of novel substituted aryl-thiazole (SAT) analogs via one-pot multi-component reaction as potent cytotoxic agents against cancer cell lines

In this study, twenty-five (25) substituted aryl thiazoles (SAT) 1–25 were synthesized, and their in vitro cytotoxicity was evaluated against four cancer cell lines, MCF-7 (ER^+ve breast), MDA-MB-231 (ER^−ve breast), HCT116 (colorectal) and HeLa (cervical). The activity was compared with the standard anticancer drug doxorubicin (IC₅₀ = 1.56 ± 0.05 μM). Among them, compounds 1, 4–8, and 19 were found to be toxic to all four cancer cell lines (IC₅₀ values 5.37 ± 0.56–46.72 ± 1.80 μM). Compound 20 was selectively active against MCF7 breast cancer cells with IC₅₀ of 40.21 ± 4.15 μM, whereas compound 19 was active against MCF7 and HeLa cells with IC₅₀ of 46.72 ± 1.8, and 19.86 ± 0.11 μM, respectively. These results suggest that substituted aryl thiazoles 1 and 4 deserve to be further investigated in vivo as anticancer leads.     

Green synthesis of silver nanoparticles by Conocarpus Lancifolius plant extract and their antimicrobial and anticancer activities

Due to drug addiction and the emergence of antibiotic resistance in pathogens, the disease load and medication intake have risen worldwide. The alternative treatment for drug-resistant infections is Nano formulation-based antimicrobial agents. The plant extract of Conocarpus Lancifolius fruits was used to synthesize silver nanoparticles in the current study, and it was further employed as an antimicrobial and anticancer agent. Nanoparticles have been characterized by UV–visible spectrometer revealed the notable peak of λ_max = 410–442 nm, which confirms the reduction of silver ion to elemental silver nanoparticles, and the biological moieties in the synthesis were further confirmed by FTIR analysis. The stability and crystalline nature of materials were approved by XRD analysis and expected the size of the nanomaterials of 21 to 173 nm analyzed by a nanophox particle-size analyzer. In vitro, synthesized materials act as an antibacterial agent against Streptococcus pneumonia and Staphylococcus aureus. The inhibition zones of 18 and 24 mm have been estimated to be antibacterial activity against both bacteria. The potency of up to 100% of AgNPs for bacterial strains was incubated overnight at 60 μg/ml. Based on our results, biogenic AgNPs reveal significant activity against fungal pathogen Rhizopusus stolonifera and Aspergillus flavus that cause leading infectious diseases. Additionally, nanomaterials were biocompatible and demonstrated the potential anticancer activities against MDA MB-231 cells after 24-hour exposure.     

Geranylated tetraoxygenated xanthones from the pericarp of Garcinia pedunculata

Three new xanthones, pedunxanthones D-F (1–3), along with ten known compounds, were isolated from a chloroform extract of the pericarp of Garcinia pedunculata. Their structures were determined using spectroscopic techniques. Cytotoxicity against HeLa and NCI-H460 cells of the isolated compounds using an SRB assay was evaluated with pedunxanthone D (1) as the most active compound (IC₅₀ 24.9 ± 0.4 and 26.1 ± 1.5 μg/ml, respectively).     

Efficacy of biogenic selenium nanoparticles against Leishmania major: In vitro and in vivo studies

Project: This study investigated the in vitro and in vivo effectiveness of biogenic selenium nanoparticles (Se NPs), biosynthesized by Bacillus sp. MSh-1, against Leishmania major (MRHO/IR/75/ER). Procedure: The 3-(4,5-dimethylthiozol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay was used to evaluate the cytotoxicity effects of the biogenic Se NPs against both promastigote and amastigote forms of L. major. In a separate in vivo experiment, we also determined the preventive and therapeutic effects of biogenic Se NPs in BALB/c mice following subcutaneous infected with L. major. Results: The MTT assays showed that the highest toxicity occurred after 72 h against both promastigote and amastigote forms of L. major. The cytotoxicity of Se NPs was higher at all incubation times (24, 48, and 72 h) against the promastigote than the amastigote form (p < 0.05). The 50% inhibitory concentrations (IC₅₀) of the Se NPs were 1.62 ± 0.6 and 4.4 ± 0.6 μg ml^?1 against the promastigote and amastigote forms, respectively, after a 72-h incubation period. Apoptosis assays showed DNA fragmentation in promastigotes treated with Se NPs. In an animal challenge, prophylactic doses of biogenic Se NPs delayed the development of localized cutaneous lesions. Moreover, daily administration of Se NPs (5 or 10 mg kg^?1 day^?1) in similarly infected BALB/c mice that had not received prophylactic doses of Se NPs also abolished the localized lesions after 14 days. Conclusion: Based on these in vitro and in vivo studies, biogenic Se NPs can be considered as a novel therapeutic agent for treatment of the localized lesions typical of cutaneous leishmaniasis.     

Cyathula prostrata ethanol extract activates the extrinsic pathway of apoptosis in HeLa and U937 cell lines

Cyathula prostrata is a medicinal plant that is used in tropical Africa, Asia and Australia to treat many ailments including rheumatic fever, dysentery, wounds and eye trouble (Burkill, 1995). Sowemimo et al. (2009) reported cytotoxicity against a cervical cancer cell line, HeLa, at a concentration of 250 μg/mL. Due to the reported cytotoxicity, the mode of cell death caused by an ethanolic C. prostrata extract was investigated. Dose–response assays were carried out using HeLa and U937 cell lines and IC₅₀ values of 100.8 μg/mL and 64.43 μg/mL, respectively, were achieved. Cisplatin was used as a positive control for all experiments. Cytotoxicity of the plant extract was not evident when treating normal peripheral blood mononuclear cells. Progression of cells through the cell cycle, apoptosis and mitochondrial membrane potential was investigated. Arrest of cells in the G0/G1 phase of the cell cycle was evident after 24 h of exposure to the plant extract in both cell lines, but not due to increases in p21 levels. Caspase 8 activation was evident and no depolarisation of the mitochondrial membrane and cytochrome c release was seen in both cell lines. Phosphatidylserine translocation was investigated and confirmed the onset of apoptosis. Thus, it is deduced that exclusive activation of the extrinsic pathway of apoptosis is caused by the treatment of HeLa and U937 cells with ethanolic C. prostrata.     

Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines

Novel riminophenazine derivatives, characterized by the presence of the basic and cumbersome quinolizidinylalkyl and pyrrolizidinylethyl moieties, have been synthesized and tested (Rema test) against Mycobacterium tuberculosis H₃₇R_v and H₃₇R_a, and six clinical isolates of Mycobacterium avium and Mycobacterium tuberculosis. Most compounds exhibited potent activity against the tested strains, resulting more active than clofazimine, isoniazid and ethambutol.The best compounds (4, 5, 12 and 13) exhibited a MIC in the range 0.82–0.86 μM against all strains of Mycobacterium tuberculosis and, with the exception of 4 a MIC around 3.3 μM versus M. avium. The corresponding values for clofazimine (CFM) were 1.06 and 4.23 μM, respectively. Cytotoxicity was evaluated against three cell lines and compound 4 displayed a selectivity index (SI) versus the human cell line MT-4 comparable with that of CFM (SI = 5.23 vs 6.4). Toxicity against mammalian Vero 76 cell line was quite lower with SI = 79.     

Biologically synthesized green silver nanoparticles from leaf extract of Vitex negundo L. induce growth-inhibitory effect on human colon cancer cell line HCT15

Nanomedicine concerns the use of precision-engineered nanomaterials to develop novel therapeutic and diagnostic modalities for human use. The present study demonstrates the efficacy of silver nanoparticles (AgNPs) biosynthesis from leaf extract of Vitex negundo L. as an antitumor agent using human colon cancer cell line HCT15. The AgNPs synthesis was determined by UV–visible spectrum and it was further characterized by field emission scanning electron microscopy (FESEM), energy-dispersive spectroscopy (EDX), transmission electron microscopy (TEM), X-ray diffraction (XRD) and fourier transform infrared spectroscopy (FTIR) analysis. The toxicity was evaluated using changes in cell morphology, cell viability, nuclear fragmentation, cell cycle and comet assay. The percentage of cell viability was determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Our results showed that biosynthesized silver nanoparticles inhibited proliferation of human colon cancer cell line HCT15 with an IC₅₀ of 20 μg/ml at 48 h incubation. AgNPs were shown to promote apoptosis as seen in the nuclear morphological examination study using propidium iodide staining and DNA fragmentation by single cell gel electrophoresis technique. Biosynthesized AgNPs arrested HCT15 cells at G₀/G₁ and G₂/M phases with corresponding decrease in S-phase. These results suggest that AgNPs may exert its antiproliferative effects on colon cancer cell line by suppressing its growth, arresting the G₀/G₁-phase, reducing DNA synthesis and inducing apoptosis.     

The use of herbs against neglected diseases: Evaluation of in vitro leishmanicidal and trypanocidal activity of Stryphnodendron rotundifolium Mart

The evaluation of the leishmanicidal and trypanocidal activity of the hydroalcoholic extract of the bark of Stryphnodendron rotundifolium Mart. (EHCSR) was carried out to find an alternative treatment for parasitic diseases. EHCSR was prepared and used at four different concentrations (1000, 500, 250, 125 μg/mL) in in vitro assays for activity against Leishmania promastigotes using the species Leishmania brasiliensis and Leishmania infantum and for trypanocidal activity using the epimastigotes of Trypanosoma cruzi. We also tested EHCSR for cytotoxicity against adhered cultured Murine J774 fibroblasts. The tests were performed in triplicate, and the percent mortality of parasites, IC₅₀ and percent toxicity were determined. With regard to anti-leishmania activity against L. infantum, there was a mean mortality of 45% at all concentrations, and against L. brasiliensis, a substantial effect was seen at 1000 μg/mL with 56.38% mortality, where the IC₅₀ values were 1338.76 and 987.35 μg/mL, respectively. Trypanocidal activity was notably high at 1000 μg/mL extract with 82.31% mortality of epimastigotes. Cytotoxicity at the highest extract concentrations of 500 and 1000 μg/mL was respectively 75.12% and 94.14%, with IC₅₀ = 190.24 μg/mL. Despite that the extract has anti-parasitic activity, its substantial cytotoxicity against fibroblasts cells makes its systemic use nonviable as a therapeutic alternative.     

Application of S-thanatin,an antimicrobial peptide derived from thanatin,in mouse model of Klebsiella pneumoniae infection

Thanatin was first discovered from the hemipteran insect Podisus maculiventris and showed a promising antimicrobial activity. Multidrug-resistant (MDR) clinical isolates of Klebsiella pneumoniae have developed resistance to current therapies. As an attempt to resolve this problem, the efficacy of thanatin and its analogues against clinical isolates of K. pneumoniae was studied in vitro and in vivo. S-thanatin showed an improved antimicrobial activity with the tested MIC values was 2–8-fold lower than those of other thanatin analogs. Antimicrobial assay indicated a high activity of S-thanatin against K. pneumoniae in vitro with MIC between 4 and 8 μg/ml. Its in vivo activity was evaluated using a K. pneumoniae-infected mice model. Adult male ICR mice were randomly grouped and given an intraperitoneal (i.p.) administration of 2 × 10¹⁰ colony-forming units of K. pneumoniae (CI 120204205). Afterwards, mouse groups were subjected to i.p. administration of saline or S-thanatin (5, 10, or 15 mg/kg). After an inspection of 72 h, the mice were finally sacrificed for analysis of in vivo bacterial growth and plasma endotoxin level. The results showed that S-thanatin administration apparently improved the survival rate and reduced the bacterial CFU from intra-abdominal fluid in mice. The plasma endotoxin level was improved as well. All above implied that S-thanatin, as an alternative, may provide a novel strategy for treating K. pneumoniae infection and other infections due to multidrug-resistant bacteria.     

Antioxidant,antibacterial and cytotoxic potential of silver nanoparticles synthesized using terpenes rich extract of Lantana camara L. leaves

Several attempts have been made for green synthesis of silver nanoparticles (AgNPs) using different plant extracts. Present study revealed that, antioxidant, antibacterial and cytotoxic AgNPs were synthesized using terpenes-rich extract (TRE) of environmentally notorious Lantana camara L. leaves. AgNPs were characterized by advanced techniques like UV–Visible and Infra red spectroscopy; XRD, SEM techniques as terpenes coated sphere shaped NPs with average diameter 425 nm. Further, on evaluation, AgNPs were found to exhibit dose – dependent antioxidant potential, good to moderate antibacterial activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa; and toxicity on Brine shrimp (A. salinanauplii) with LD₅₀ value 514.50 µg/ml.     

Picrasin K,a new quassinoid from Quassia amara L. (Simaroubaceae)

A new quassinoid Picrasin K 1 was isolated from a decoction made of Quassia amara leaves, traditionally used in French Guyana to treat malaria. The structure and relative stereochemistry of 1 was determined through extensive NMR analysis. Picrasin K showed a low activity against Plasmodium falciparum in vitro (IC₅₀ = 8 μM), and a similar low activity on human cancerous cells line (IC₅₀ = 7 μM on MCF-7 cells line).     

Discovery of a nanomolar inhibitor of lung adenocarcinoma in vitro

Efficient methods for the preparation of 5′-substituted 5′-amino-5′-deoxy-N⁶-ureidoadenosine derivatives are described. Compounds were screened for antiproliferative activity against a panel of murine and human cell lines (L1210, CEM, and HeLa) and/or against the NCI-60. The most potent derivative inhibited the lung adenocarcinoma cell line NCI-H522 at low nanomolar concentrations (GI₅₀ = 9.7 nM).